Behavioural and electrocortical power spectrum effects of 5-methoxytryptoline and other analogs after intraventricular administration in rats.

Abstract:

:The behavioural and electrocortical power spectrum effects of tryptoline and the 5-hydroxy and 5-methoxy derivatives were studied after microinjection of the drugs into the third cerebral ventricle in freely moving rats. The three compounds produced a dose-dependent desynchronication in electrocortical activity with a concomitant syndrome of behavioural stimulation. The most potent compound was 5-methoxytryptoline, already active at 4 nmol. When given into the third cerebral ventricle, 5-methoxytryptoline antagonized the sedation and hypothermia induced by reserpine. The relative order of potencies was 5-methoxytryptoline greater than 5-hydroxytryptoline greater than tryptoline. Melatonin, the 5-methoxy-N-acetyl derivative of serotonin, when injected into the third cerebral ventricle, did not produce desynchronization and elicited only mild sedation. The high potency of 5-methoxytryptoline following injection into the third cerebral ventricle and the relative order of potencies with 5-hydroxytryptoline and tryptoline is compared to the affinity of these compounds for the modulatory site of the serotonin transporter which was labelled with [3H]imipramine or [3H]paroxetine.

journal_name

Eur J Pharmacol

authors

Nistico G,De Sarro GB,Langer SZ

doi

10.1016/0014-2999(87)90660-1

subject

Has Abstract

pub_date

1987-10-06 00:00:00

pages

121-8

issue

1

eissn

0014-2999

issn

1879-0712

pii

0014-2999(87)90660-1

journal_volume

142

pub_type

杂志文章
  • Felbamate inhibits cloned voltage-dependent Na+ channels from human and rat brain.

    abstract::The novel antiepileptic and neuroprotective drug felbamate (1 mM) caused a marked inhibition of voltage-dependent Na+ currents expressed in Xenopus oocytes upon injection of the cRNA encoding alpha-subunits from rat and human brain. This inhibition was present only if felbamate was perfused on the intracellular side o...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(96)00802-3

    authors: Taglialatela M,Ongini E,Brown AM,Di Renzo G,Annunziato L

    更新日期:1996-12-05 00:00:00

  • Under explored epigenetic modulators: role in glioma chemotherapy.

    abstract::Patients with somatic mutations of epigenetic regulators are characterized by aberrant chromatin modification patterns. Recent mechanistic studies pairing chemical tool compounds and deep-sequencing technology have greatly broadened our understanding of epigenetic regulation in glioma progression and underpinned alter...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2018.05.047

    authors: Chen YH,Zeng WJ,Wen ZP,Cheng Q,Chen XP

    更新日期:2018-08-15 00:00:00

  • Depletions of central norepinephrine by intraventricular xylamine in rats.

    abstract::A series of neurochemical studies evaluated the selectivity of the depletions of norepinephrine produced by intraventricular injections of xylamine. Brain monoamines were assayed by liquid chromatography with electrochemical detection. With ether anesthesia, bilateral injections of 50 or 100 micrograms xylamine reduce...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(84)90228-0

    authors: Geyer MA,Gordon J,Adams LM

    更新日期:1984-04-20 00:00:00

  • Inhibition of membrane currents and rises of intracellular Ca2+ in PC12 cells by CGS 9343B, a calmodulin inhibitor.

    abstract::The calmodulin inhibitor 1,3-dihydro-1-[1-((4-methyl-4H,6H-pyrrolo[1,2-a]-[4,1]benzoxazepin - 4-yl)methyl)-4-piperidinyl]-2H-benzimidazol-2-one maleate (CGS 9343B) caused a reversible block of voltage-activated Ca2+, Na+, and K+ currents in differentiated rat pheochromocytoma (PC12) cells. The drug also inhibited nico...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(92)90182-u

    authors: Neuhaus R,Reber BF

    更新日期:1992-06-05 00:00:00

  • Specific and potent interactions of carbamazepine with brain adenosine receptors.

    abstract::Carbamazepine, a drug effective in pain, seizure, and affective disorders, was screened for its ability to interact with a variety of neurotransmitter and neuromodulator binding sites on brain membranes. The most potent effect was observed on adenosine antagonist ( [3H]DPX) binding to the adenosine receptor (KI = 3.5 ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90135-8

    authors: Marangos PJ,Post RM,Patel J,Zander K,Parma A,Weiss S

    更新日期:1983-09-30 00:00:00

  • In vitro stimulation of insulin release by SL 84.0418, a new alpha 2-adrenoceptor antagonist.

    abstract::SL 84.0418 (2-(4,5-dihydro-1H-imidazol-2-yl)-1,2,4,5-tetrahydro-2-propyl-pyrrolo[3, 2,1- hi]-indole hydrocholoride) is a novel alpha 2-adrenoceptor antagonist which possesses anti-hyperglycaemic properties in vitro study, we tested its effects on insulin release from isolated mouse islets. In the presence of 15 mM glu...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90366-2

    authors: Jonas JC,Plant TD,Angel I,Langer SZ,Henquin JC

    更新日期:1994-03-11 00:00:00

  • Suppression by cetirizine of pleurisy triggered by antigen in actively sensitized rats.

    abstract::The efficacy of cetirizine in comparison with meclizine, another piperazine H1 receptor antagonist, in rat pleurisy caused by allergen or autacoid was investigated. Sensitization was achieved by subcutaneous injection of a mixture of ovalbumin and aluminium hydroxide. Fourteen days later, the animals were challenged w...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(92)90811-h

    authors: Pasquale CP,e Silva PM,Lima MC,Diaz BL,Rihoux JP,Vargaftig BB,Cordeiro RS,Martins MA

    更新日期:1992-11-13 00:00:00

  • Reversal of alpha-adrenoceptor blockade by propranolol in isolated rat pulmonary artery.

    abstract::Pulmonary artery rings were prepared from rats (group I to VI, n = 5-7 per group) in order to investigate if a beta-adrenoceptor antagonist interferes with the effect of alpha-adrenoceptor blockade. In I, four cumulative noradrenaline (NA) dose-response curves (10(-9) to 10(-3) M) were constructed. In II, NA curves we...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)90247-4

    authors: Abdelrahman A,Nguyen H,Pang CC

    更新日期:1990-05-31 00:00:00

  • Activation of KCNQ5 channels stably expressed in HEK293 cells by BMS-204352.

    abstract::The novel anti-ischemic compound, BMS-204352 ((3S)-(+)-(5-chloro-2-methoxyphenyl)-1,3-dihydro-3-fluoro-6-(trifluoromethyl)-2H-indol-2-one)), strongly activates the voltage-gated K+ channel KCNQ5 in a concentration-dependent manner with an EC50 of 2.4 microM. At 10 microM, BMS-204352 increased the steady state current ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)01287-6

    authors: Dupuis DS,Schrøder RL,Jespersen T,Christensen JK,Christophersen P,Jensen BS,Olesen SP

    更新日期:2002-02-22 00:00:00

  • In vitro and in vivo functional profile characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3-carboxamido)morphinan (NAQ) as a low efficacy mu opioid receptor modulator.

    abstract::Evidence has shown that downstream signaling by mu opioid receptor (MOR) agonists that recruit β-arrestin2 may lead to the development of tolerance. Also, it has been suggested that opioid receptor desensitization and cyclic AMP overshoot contributes to the development of tolerance and occurrence of withdrawal, respec...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2018.03.013

    authors: Obeng S,Yuan Y,Jali A,Selley DE,Zhang Y

    更新日期:2018-05-15 00:00:00

  • Anticancer effects and possible mechanisms of lycopene intervention on N-methylbenzylnitrosamine induced esophageal cancer in F344 rats based on PPARγ1.

    abstract::Lycopene, a natural carotenoid, has potential chemopreventive effects in many cancers. This study aimed to examine the effects of lycopene on regulating the inflammation and apoptosis of N-nitrosomethylbenzylamine(NMBzA) induced esophageal cancer in F344 rats. After the rats were fed normal diets containing different ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173230

    authors: Cui L,Xu F,Wu K,Li L,Qiao T,Li Z,Chen T,Sun C

    更新日期:2020-08-15 00:00:00

  • Cobalt(II) β-ketoaminato complexes as novel inhibitors of neuroinflammation.

    abstract::Neuroinflammation contributes to the pathogenesis of neurological disorders including stroke, head trauma, multiple sclerosis, amyotrophic lateral sclerosis as well as age-associated neurodegenerative disorders including Alzheimer's and Parkinson's diseases. Therefore, anti-inflammatory drugs could be used to slow the...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.11.038

    authors: Madeira JM,Beloukhina N,Boudreau K,Boettcher TA,Gurley L,Walker DG,McNeil WS,Klegeris A

    更新日期:2012-02-15 00:00:00

  • Correlation between neuroleptic binding to sigma(1) and sigma(2) receptors and acute dystonic reactions.

    abstract::Acute dystonic reactions are motor side effects that occur soon after the initiation of neuroleptic treatment. Although earlier studies indicate that these abnormal movements can be induced in animals and humans via activation of sigma receptors, the relative contribution of the different sigma receptor subtypes is un...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00430-1

    authors: Matsumoto RR,Pouw B

    更新日期:2000-08-04 00:00:00

  • The interaction between vigabatrin and diazepam on the electroencephalogram during active behaviour in rats: an isobolic analysis.

    abstract::To test whether polytherapy with two gamma-aminobutyric acid (GABA) -ergic drugs might be clinically relevant for epilepsy treatment, effects on spike and wave discharges, the fraction of time spent being behaviourally active, and the background electroencephalogram (EEG) during behavioural activity of vigabatrin (15-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2004.05.027

    authors: Bouwman BM,Heesen E,van Rijn CM

    更新日期:2004-07-14 00:00:00

  • Ryanodine-induced contraction in femoral artery from spontaneously hypertensive rats.

    abstract::The mechanisms of ryanodine-induced contractions were studied in strips of femoral arteries from spontaneously hypertensive rats (SHR) and normotensive Wistar-Kyoto rats (WKY). Ryanodine (30 nM to 30 microM) alone contracted arterial strips in a dose-dependent manner. The maximum contraction in SHR was about 5 times g...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90383-2

    authors: Kojima M,Dohi Y,Sato K

    更新日期:1994-03-11 00:00:00

  • The regulation of mitochondrial respiration by opening of mKCa channels is age-dependent.

    abstract::The protective potency of ischemic preconditioning decreases with increasing age. A key step in ischemic preconditioning is the opening of mitochondrial Ca(2+) sensitive K(+) (mK(Ca)) channels, which causes mild uncoupling of mitochondrial respiration. We hypothesized that aging reduces the effects of mK(Ca) channel o...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2007.09.008

    authors: Heinen A,Winning A,Schlack W,Hollmann MW,Preckel B,Frässdorf J,Weber NC

    更新日期:2008-01-14 00:00:00

  • Chronic mianserin treatment decreases 5-HT2 receptor binding without altering 5-HT2 receptor mRNA levels.

    abstract::Rats were injected with 15 mg/kg (i.p.) mianserin or vehicle (saline) for 4, 10 or 21 days and 5-HT2 receptor binding and mRNA levels measured. Treatment with mianserin induced a substantial decrease in 5-HT2 radioligand binding (44-59% decrease; P less than 0.05 vs. control). No changes in the amount of 5-HT2 or, as ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(91)90093-w

    authors: Roth BL,Ciaranello RD

    更新日期:1991-06-19 00:00:00

  • Effects of AY-22,241 (Actodigin) on electrical and mechanical activity of cardiac tissues.

    abstract::AY-22,241 (Actodigin) is a new rapid-acting semisynthetic cardiotonic steroid. In experiments on contractility of cat papillary muscle, Actodigin (2 times 10(-7) to 4 times 10(-6) M) produced a dose-dependent positive inotropic effect, a marked increase in the maximum rate of force development, and no change in restin...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(75)90316-7

    authors: Gliklich JI,Gaffney R,Rosen MR,Hoffman BF

    更新日期:1975-05-01 00:00:00

  • A re-examination of the GABA-inhibitory action of bicuculline on lobster muscle.

    abstract::The GABA-inhibitory action of bicuculline on lobster muscle was critically re-examined. Bicuculline (20-100 micrometers) depressed the GABA-evoked conductance increase in a reversible manner, the double reciprocal transformation of the GABA dose/conductance curves remaining linear. If bicuculline was assumed to be a p...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(81)90428-3

    authors: Smart TG,Constanti A

    更新日期:1981-03-05 00:00:00

  • Pharmacological studies with a nonpeptidic, delta-opioid (-)-(1R,5R,9R)-5,9-dimethyl-2'-hydroxy-2-(6-hydroxyhexyl)-6,7-benzomorphan hydrochloride ((-)-NIH 11082).

    abstract::In the search for a selective delta-opioid receptor agonist, (-)-(1R,5R,9R)-5,9-dimethyl-2'-hydroxy-2-(6-hydroxyhexyl)-6,7-benzomorphan hydrochloride ((-)-NIH 11082) and the (+)-enantiomer were synthesized and tested. (-)-NIH 11082 displayed antinociceptive activity in the paraphenylquinone test (PPQ test) in male ICR...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2007.03.008

    authors: Aceto MD,May EL,Harris LS,Bowman ER,Cook CD

    更新日期:2007-07-02 00:00:00

  • cAMP-Dependent potentiation of the Ca(2+)-activated release of the anionic fluorescent dye, calcein, from rat parotid acinar cells.

    abstract::A recent study indicates that elevation of [Ca(2+)](i) enhances the release of calcein, an anionic fluorescent dye, from isolated exocrine acinar cells, so cytoplasmic calcein is useful for monitoring the secretion of organic anions. In this study, we investigated the effect of cAMP on the calcein release evoked by el...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00898-5

    authors: Sugita M,Hirono C,Furuya K,Yamagishi S,Kanno Y,Shiba Y

    更新日期:2000-02-04 00:00:00

  • Functional identification of alpha 1-adrenoceptor subtypes in human prostate: comparison with those in rat vas deferens and spleen.

    abstract::The effects of some alpha 1-adrenoceptor antagonists (prazosin, nonselective for the alpha 1A- and alpha 1B-adrenoceptor subtypes; 5-methyl-urapidil, selective for the alpha 1A-adrenoceptor subtype; chloroethylclonidine, selective for the alpha 1B-adrenoceptor subtype) and nifedipine were compared on contractile respo...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90223-2

    authors: Teng CM,Guh JH,Ko FN

    更新日期:1994-11-14 00:00:00

  • Brain α4β2 nicotinic acetylcholine receptors are involved in the secretion of noradrenaline and adrenaline from adrenal medulla in rats.

    abstract::Recently, we reported that intracerebroventricularly (i.c.v.) administered (±)-epibatidine (a non-selective agonist of nicotinic acetylcholine receptors) elevates plasma noradrenaline and adrenaline through brain nicotinic acetylcholine receptor-mediated mechanisms in rats. In the present study, we characterized the r...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2010.12.034

    authors: Shimizu T,Tanaka K,Hasegawa T,Yokotani K

    更新日期:2011-03-11 00:00:00

  • Dopamine agonist-induced hyperglycemia in rats: structure-activity relationships and mechanisms of action.

    abstract::The concentration of blood glucose was measured in rats after administration of a number of drugs characterized as dopamine agonists. Compounds that cause release of dopamine, or agents that block the reuptake of dopamine, did not elevate blood glucose. Some direct dopamine receptor stimulants (lergotrile, bromocripti...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90234-0

    authors: Schmidt MJ,Root MA,Hall JL

    更新日期:1983-06-03 00:00:00

  • Effects of idazoxan on dorsal raphe 5-hydroxytryptamine neuronal function.

    abstract::The effects of the alpha 2-adrenoceptor antagonist idazoxan on 5-hydroxytryptamine (5-HT) neuronal firing and release have been investigated. Idazoxan, administered i.v. (10 micrograms/kg and 0.5 mg/kg) increased dorsal raphe nucleus (DRN)-5-HT neuronal firing rate in a dose-dependent fashion. At the higher dose, a vo...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(91)90204-4

    authors: Garratt JC,Crespi F,Mason R,Marsden CA

    更新日期:1991-01-25 00:00:00

  • The inotropic effects of a synthetic pyrethroid decamethrin on isolated guinea pig atrial muscle.

    abstract::Pyrethroid insecticides have been reported to increase transmembrane sodium influx and inhibit ion-dependent ATPases in insect, squid, and toad nerve tissues. Since changes in sarcolemmal ion fluxes and inhibition of membrane-bound ATPases can alter myocardial contractility, the effects of a potent synthetic pyrethroi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(84)90279-6

    authors: Berlin JR,Akera T,Brody TM,Matsumura F

    更新日期:1984-03-02 00:00:00

  • Vespula vulgaris venom: role of kinins and release of 5-hydroxytryptamine from skin mast cells.

    abstract::Wasp venoms contain several active components, among them kinin-related peptides. Like bradykinin and [Thr6]bradykinin, Vespula vulgaris venom caused paw oedema following subplantar injection in anaesthetized rats. The oedema was partly inhibited by the bradykinin B2 receptor antagonist icatibant (Hoe 140); the remain...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00276-3

    authors: Griesbacher T,Althuber P,Zenz M,Rainer I,Griengl S,Lembeck F

    更新日期:1998-06-12 00:00:00

  • Neuroprotective effect of WIN 55,212-2 pretreatment against focal cerebral ischemia through activation of extracellular signal-regulated kinases in rats.

    abstract::It is well documented that cannabinoid receptor agonist WIN 55,212-2 had protective effect against cerebral ischemic injury. Our previous study indicated that WIN 55,212-2 pretreatment induced ischemic tolerance to focal cerebral ischemia in a dose-dependent manner. The aim of the present study was to investigate the ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2010.07.024

    authors: Hu B,Wang Q,Chen Y,Du J,Zhu X,Lu Y,Xiong L,Chen S

    更新日期:2010-10-25 00:00:00

  • Pharmacology of ectonucleotidases: relevance for the treatment of cardiovascular disorders.

    abstract::ATP and other extracellular nucleotides have diverse and potent effects in different organs. Evidence indicates that extracellular nucleotides and nucleosides deliver crucial signals by acting upon a wide variety of purinergic receptors, which include 19 members separated in three families. Purinergic receptors encomp...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.09.003

    authors: Mathieu P

    更新日期:2012-12-05 00:00:00

  • Examination of the effect of the cannabinoid receptor agonist, CP 55,940, on electrically evoked transmitter release from rat brain slices.

    abstract::In the present study we examined the effect of the cannabinoid receptor agonist, [[1 a,2-(R)-5-(1,1-dimethylheptyl)-2-[5-hydroxy-2-(3-hydroxypropyl)cyc lohexyl]-phenol; CP 55,940] on [14C]acetylcholine and [3H]norepinephrine release from hippocampal slices and on [14C]acetylcholine release from striatal slices. CP 55,...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(97)00082-4

    authors: Gifford AN,Samiian L,Gatley SJ,Ashby CR Jr

    更新日期:1997-04-18 00:00:00